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Literature DB >> 8170948

Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells.

J F Mayaux¹, A Bousseau, R Pauwels, T Huet, Y Hénin, N Dereu, M Evers, F Soler, C Poujade, E De Clercq.

Abstract

A series of triterpene compounds characterized by a stringent structure-activity relationship were identified as potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) replication. Currently studied botulinic derivatives have 50% inhibitory concentrations (IC50) against HIV-1 strain IIIB/LAI in the 10 nM range in several cellular infection assays but are inactive against HIV-2. These compounds did not significantly inhibit the in vitro activities of several purified HIV-1 enzymes. Rather, they appeared to block virus infection at a postbinding, envelope-dependent step involved in the fusion of the virus to the cell membrane.

Entities: Chemical Disease Species

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Year: 1994 PMID： 8170948 PMCID： PMC43620 DOI： 10.1073/pnas.91.9.3564

Source DB: PubMed Journal: Proc Natl Acad Sci U S A ISSN： 0027-8424 Impact factor: 11.205

28 in total

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